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ERAP has been crystallized in two different
2024-11-28

ERAP1 has been crystallized in two different conformations, wherein the C-terminal domain IV is either closely interacting with domains I/II and enclosing the active site (termed ‘closed’), or is rotated away in a hinge motion which exposes the active site (‘open’). This large motion correlates with
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br Results and discussion br Conclusion The
2024-11-28

Results and discussion Conclusion The tyrosine kinase ALK represents one of the most successful molecular targets for the development of precise medicine to treat stratified subgroups of cancer patients. Three generations of ALK inhibitors have been awarded the FDA's approval or are being exte
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We next considered the effect of alkyl chain length on
2024-11-28

We next considered the effect of alkyl chain length on the inhibitory activity. As can be seen from , it is obvious that there is no proportional relationship between the methylene chain length and activity. The activity decreased when the chain length increased from 1 to 3 and increased with elonga
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br Materials and methods br Results br Discussion Knowledge
2024-11-28

Materials and methods Results Discussion Knowledge of the molecular basis of an inherited genetic disease is crucial for understanding the disease pathology and, ultimately, for therapeutic design. Several recent reports have stressed the need for physical characterization of disease-associ
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Various compounds have been designed
2024-11-28

Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic cck 1303 moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to be a poten
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Pregnane X receptor PXR is a
2024-11-28

Pregnane X receptor (PXR) is a nuclear receptor that plays an important role in regulation of metabolism and disposition of structurally diverse xenobiotics as well as endogenous steroids and bile acids (Bertilsson et al., 1998, Kliewer et al., 1998, Lehmann et al., 1998). PXR regulates the metaboli
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We now present a series of findings obtained in heterologous
2024-11-28

We now present a series of findings obtained in heterologous expression systems, brain slices, and living animals that suggest that any interaction between mGlu7 and α1-adrenergic receptors exists, is specific, and is physiologically and behaviourally relevant. Materials and methods Norepinephri
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Tubastatin A HCl br Conclusion The HT receptor family is com
2024-11-28

Conclusion The 5-HT receptor family is complex, and one may ask as does Bryan Roth et al. [205] whether this is useless Tubastatin A HCl (i.e. too much redundancy) or an embarrassment of the riches (i.e. many potential targets to choose from to affect normal or pathological function); molecular
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Multiple ASD susceptibility genes converge on cellular
2024-11-27

Multiple ASD susceptibility genes converge on cellular pathways that intersect at the postsynaptic site of glutamatergic synapses (Bourgeron, 2015; Peca & Feng, 2012), the development and maturation of synaptic contacts (Gilman et al., 2011) or synaptic transmission (Li et al., 2014). The majority o
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A correlation analysis was performed to
2024-11-27

A correlation analysis was performed to investigate a possible relationship between serum resistin levels and MG-ADL. We observed a significant relationship between serum resistin levels and MG-ADL scores in AChR-GMG-positive cases (r=0.285, p=0.032; Fig. 1C). There were also significant correlation
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Anti LT therapy by LO inhibition
2024-11-27

Anti-LT therapy by 5-LO inhibition has been hampered by occurring liver toxicities by Zileuton or the clinical phase II compound Atreleuton [36], [37] However both compounds possess a thiophene as well as an N-hydroxyurea moiety. These features could be linked with reactive thiophene intermediates [
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br Conflicts of interest br Acknowledgments The authors ackn
2024-11-27

Conflicts of interest Acknowledgments The authors acknowledge National Institute for Medical Research Development (NIMAD) project no. 940943 and National Research Institute for Science Policy (NRISP) no. 1456 for financial support of this work. AM appreciates National Institute for Genetic En
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br Regulation of V ATPase assembly in response to
2024-11-27

Regulation of V-ATPase assembly in response to changes in amino Aldicarb levels A central regulator of cell growth and metabolism is mTORC1 [38]. mTORC1 integrates signals from nutrient availability and growth factor receptors to control such processes as protein and lipid synthesis and autophag
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For the TSH receptor signaling at the Golgi
2024-11-27

For the TSH receptor, signaling at the Golgi/trans-Golgi network appears required for both rapid effects of TSH − such as PD0332991 Isethionate depolymerization, which is implicated in thyroglobulin reuptake and, thus, thyroid hormone release − and late ones, such as those on gene transcription. Co
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br Introduction O Dowd et
2024-11-27

Introduction O’Dowd et al. identified a gene very similar to angiotensin type-1 receptor in 1993 (O’Dowd et al., 1993). The specific selective ligand of this receptor called APJ receptor was determined by Tatemoto et al. in 1998 as apelin (Tatemoto et al., 1998). The high expression of apelin and
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